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Optimization of 7-alkene-3-quinolinecarbonitriles as Src kinase inhibitors |
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| Authors: | Diane H. Boschelli Daniel Wang Yan Wang Biqi Wu Erick E. Honores Ana Carolina Barrios Sosa Inder Chaudhary Jennifer Golas Judy Lucas Frank Boschelli |
| Affiliation: | 1. Wyeth Research, Chemical Sciences 401 N. Middletown Road, Pearl River, NY 10965, United States;2. Wyeth Research, Drug Safety and Metabolism 401 N. Middletown Road, Pearl River, NY 10965, United States;3. Wyeth Research, Oncology 401 N. Middletown Road, Pearl River, NY 10965, United States |
| Abstract: | The 7-alkene-3-quinolinecarbonitrile 20, a potent inhibitor of Src enzymatic and cellular activity with IC50 values of 2.1 and 58 nM, respectively, had comparable efficacy to bosutinib in a colon tumor xenograft study. |
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